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Related Concept Videos

Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

Chemotherapy-Induced Nausea and Vomiting: Cannabinoids

Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

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Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents
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Published on: August 22, 2025

Endocannabinoid receptor pharmacology.

Betty Yao1, Ken Mackie

  • 1Neuroscience Research, Abbott Laboratories, Abbott Park, IL 60048, USA. betty.yao@abbott.com

Current Topics in Behavioral Neurosciences
|November 25, 2010
PubMed
Summary

This chapter reviews the pharmacology of endocannabinoid receptors, focusing on G-protein-coupled receptors (GPCRs) and their signaling pathways. It covers receptor agonists, antagonists, and future research directions in endocannabinoid signaling.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Molecular Biology

Background:

  • Endocannabinoid receptors are primarily G-protein-coupled receptors (GPCRs).
  • Understanding GPCR signaling is fundamental to cannabinoid receptor function.
  • This chapter provides foundational knowledge for advanced topics in endocannabinoid signaling.

Purpose of the Study:

  • To review the basic pharmacology of endocannabinoid receptors.
  • To focus on G-protein-coupled receptors (GPCRs) as the primary cannabinoid receptors.
  • To introduce the essential pharmacology for understanding endocannabinoid signaling.

Main Methods:

  • Review of GPCR signaling mechanisms.
  • Presentation of cannabinoid receptor signaling features and effectors.

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  • Discussion of cannabinoid receptor agonists and antagonists.

    • Main Results:

    • Detailed explanation of GPCR signaling pathways relevant to cannabinoid receptors.
    • Identification of key effectors modulated by cannabinoid receptor activation.
    • Overview of pharmacological tools (agonists and antagonists) for studying cannabinoid receptors.

    Conclusions:

    • A comprehensive understanding of GPCR signaling is crucial for cannabinoid receptor pharmacology.
    • Cannabinoid receptors modulate various cellular effectors through GPCR pathways.
    • Pharmacological agents targeting cannabinoid receptors are vital for research and therapeutic development.